JP2005501013A - Gaba類似体の全身濃度が持続するアミノ酸コンジュゲート - Google Patents

Gaba類似体の全身濃度が持続するアミノ酸コンジュゲート Download PDF

Info

Publication number
JP2005501013A
JP2005501013A JP2003503171A JP2003503171A JP2005501013A JP 2005501013 A JP2005501013 A JP 2005501013A JP 2003503171 A JP2003503171 A JP 2003503171A JP 2003503171 A JP2003503171 A JP 2003503171A JP 2005501013 A JP2005501013 A JP 2005501013A
Authority
JP
Japan
Prior art keywords
substituted
alkyl
aryl
heteroaryl
cycloalkyl
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
JP2003503171A
Other languages
English (en)
Japanese (ja)
Other versions
JP2005501013A5 (enExample
Inventor
ギャロップ,マーク・エイ
カンディ,ケネス・シー
シューアマン,ランドール・エイ
バレット,ロナルド・ダブリュー
ゼランゲ,ノア
Original Assignee
ゼノポート,インコーポレイテッド
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by ゼノポート,インコーポレイテッド filed Critical ゼノポート,インコーポレイテッド
Publication of JP2005501013A publication Critical patent/JP2005501013A/ja
Publication of JP2005501013A5 publication Critical patent/JP2005501013A5/ja
Pending legal-status Critical Current

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/62—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/32—Alcohol-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/12—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atom of at least one of the carboxamide groups bound to an acyclic carbon atom of a hydrocarbon radical substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/20—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/44—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton
    • C07C317/48—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C317/50—Sulfones; Sulfoxides having sulfone or sulfoxide groups and carboxyl groups bound to the same carbon skeleton the carbon skeleton being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/57—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C323/58—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton
    • C07C323/59—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups with amino groups bound to the carbon skeleton with acylated amino groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/53—Immunoassay; Biospecific binding assay; Materials therefor
    • G01N33/566—Immunoassay; Biospecific binding assay; Materials therefor using specific carrier or receptor proteins as ligand binding reagents where possible specific carrier or receptor proteins are classified with their target compounds
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Molecular Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Biochemistry (AREA)
  • Pain & Pain Management (AREA)
  • Addiction (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Physics & Mathematics (AREA)
  • Biophysics (AREA)
  • Epidemiology (AREA)
  • Pathology (AREA)
  • Biotechnology (AREA)
  • Cell Biology (AREA)
  • General Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Analytical Chemistry (AREA)
  • Food Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Rheumatology (AREA)
JP2003503171A 2001-06-11 2002-06-11 Gaba類似体の全身濃度が持続するアミノ酸コンジュゲート Pending JP2005501013A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US29773201P 2001-06-11 2001-06-11
US36461902P 2002-03-18 2002-03-18
PCT/US2002/018493 WO2002100344A2 (en) 2001-06-11 2002-06-11 Amino acid conjugates providing for sustained systemic concentrations of gaba analogues

Publications (2)

Publication Number Publication Date
JP2005501013A true JP2005501013A (ja) 2005-01-13
JP2005501013A5 JP2005501013A5 (enExample) 2006-01-05

Family

ID=31498147

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2003503171A Pending JP2005501013A (ja) 2001-06-11 2002-06-11 Gaba類似体の全身濃度が持続するアミノ酸コンジュゲート

Country Status (5)

Country Link
US (3) US7420002B2 (enExample)
EP (1) EP1412324A4 (enExample)
JP (1) JP2005501013A (enExample)
AU (1) AU2002345638A1 (enExample)
WO (1) WO2002100344A2 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007506729A (ja) * 2003-09-25 2007-03-22 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー α2δタンパク質に親和性を有するアミノ酸のプロドラッグ
US8251059B2 (en) 2006-06-27 2012-08-28 Otsuka Pharmaceutical Co., Ltd. Powder inhaler
JP2013518897A (ja) * 2010-02-03 2013-05-23 エムイーエイチ アソシエイツ,インコーポレイテッド 選択的および生体活性的等配電子体としての多重置換フルオロメタン

Families Citing this family (29)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4342934B2 (ja) * 2001-06-11 2009-10-14 キセノポート インコーポレーティッド Pept−2輸送体を介した薬剤の投与
US6818787B2 (en) 2001-06-11 2004-11-16 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
EP1412324A4 (en) * 2001-06-11 2004-09-29 Xenoport Inc AMINO ACID CONJUGATES THAT RESULT IN GABA ANALOGA LASTING SYSTEMIC CONCENTRATIONS
US7186855B2 (en) 2001-06-11 2007-03-06 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
US7232924B2 (en) 2001-06-11 2007-06-19 Xenoport, Inc. Methods for synthesis of acyloxyalkyl derivatives of GABA analogs
US8048917B2 (en) 2005-04-06 2011-11-01 Xenoport, Inc. Prodrugs of GABA analogs, compositions and uses thereof
TWI312285B (en) 2001-10-25 2009-07-21 Depomed Inc Methods of treatment using a gastric retained gabapentin dosage
US7612112B2 (en) 2001-10-25 2009-11-03 Depomed, Inc. Methods of treatment using a gastric retained gabapentin dosage
KR100747464B1 (ko) * 2002-01-05 2007-08-09 엘지전자 주식회사 고속하향링크패킷접속(hsdpa)시스템을 위한타이머를 이용한 교착상황 회피방법
AU2003215024B2 (en) 2002-03-26 2008-02-21 Merck Sharp & Dohme Corp. Spirocyclic amides as cannabinoid receptor modulators
WO2003094842A2 (en) * 2002-05-07 2003-11-20 A & D Bioscience, Inc. Conjugates comprising central nervous system active drug
WO2003099338A2 (en) * 2002-05-17 2003-12-04 Xenoport, Inc. Amino acid conjugates providing for sustained systemic concentrations of gaba analogues
US8173840B2 (en) * 2003-07-29 2012-05-08 Signature R&D Holdings, Llc Compounds with high therapeutic index
US7589233B2 (en) * 2003-07-29 2009-09-15 Signature R&D Holdings, Llc L-Threonine derivatives of high therapeutic index
CA2538802C (en) 2003-09-17 2015-01-27 Xenoport, Inc. Treating or preventing restless legs syndrome using prodrugs of gaba analogs
RU2006118801A (ru) * 2003-10-31 2007-12-10 Алза Корпорейшн (Us) Композиции и лекарственные формы для усиления всасывания габапентина и прегабалина
FR2883873B1 (fr) 2005-03-31 2009-07-10 Pharmamens Sarl Inhibiteurs d'age
US20090176882A1 (en) 2008-12-09 2009-07-09 Depomed, Inc. Gastric retentive gabapentin dosage forms and methods for using same
US8828665B2 (en) 2007-02-16 2014-09-09 Ark Diagnostics, Inc. Compounds and methods for use in detecting gabapentin
SG157299A1 (en) 2008-05-09 2009-12-29 Agency Science Tech & Res Diagnosis and treatment of kawasaki disease
US8168756B2 (en) 2008-10-24 2012-05-01 Ark Diagnostics, Inc. Levetiracetam immunoassays
US20110130454A1 (en) * 2009-11-24 2011-06-02 Xenoport, Inc. Prodrugs of gamma-amino acid, alpha-2-delta ligands, pharmaceutical compositions and uses thereof
US20110124705A1 (en) * 2009-11-24 2011-05-26 Xenoport, Inc. Prodrugs of alpha-2-delta ligands, pharmaceutical compositions and uses thereof
CN107050456B (zh) 2010-09-28 2022-08-12 加利福尼亚大学董事会 治疗代谢综合征相关疾病的gaba激动剂和治疗或预防i型糖尿病的gaba组合
WO2012144551A1 (ja) 2011-04-20 2012-10-26 財団法人乙卯研究所 ケイ素含有カルボン酸誘導体
JP5572783B1 (ja) 2012-10-18 2014-08-13 有限会社ケムフィズ ケイ素含有カルボン酸誘導体
WO2014113717A1 (en) 2013-01-18 2014-07-24 Ark Diagnostics, Inc. Voriconazole immunoassays
WO2014126861A1 (en) 2013-02-13 2014-08-21 Ark Diagnostics, Inc. Posaconazole immunoassays
CN105997970A (zh) * 2015-12-16 2016-10-12 南昌大学 γ-氨基丁酸在制备胃粘膜保护剂中的应用

Family Cites Families (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2996431A (en) * 1953-12-16 1961-08-15 Barry Richard Henry Friable tablet and process for manufacturing same
US3402240A (en) * 1957-06-25 1968-09-17 Pfizer & Co C Medicinal tablet and process of making same
US3139383A (en) * 1961-06-26 1964-06-30 Norton Co Encapsulated time release pellets and method for encapsulating the same
SU298556A1 (enExample) 1969-12-25 1971-06-10 Л. А. Вакусевич , О. В. Давыдова
US3962414A (en) * 1972-04-27 1976-06-08 Alza Corporation Structured bioerodible drug delivery device
US3845770A (en) * 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3811444A (en) * 1972-12-27 1974-05-21 Alza Corp Bioerodible ocular device
US3916899A (en) * 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
DE2336218C3 (de) * 1973-07-17 1985-11-14 Byk Gulden Lomberg Chemische Fabrik Gmbh, 7750 Konstanz Orale Arzneiform
US3992518A (en) * 1974-10-24 1976-11-16 G. D. Searle & Co. Method for making a microsealed delivery device
GB1478759A (en) * 1974-11-18 1977-07-06 Alza Corp Process for forming outlet passageways in pills using a laser
DE2460891C2 (de) * 1974-12-21 1982-09-23 Gödecke AG, 1000 Berlin 1-Aminomethyl-1-cycloalkanessigsäuren und deren Ester, Verfahren zu deren Herstellung und diese Verbindungen enthaltende Arzneimittel
US4087544A (en) * 1974-12-21 1978-05-02 Warner-Lambert Company Treatment of cranial dysfunctions using novel cyclic amino acids
US4093709A (en) * 1975-01-28 1978-06-06 Alza Corporation Drug delivery devices manufactured from poly(orthoesters) and poly(orthocarbonates)
US4063064A (en) * 1976-02-23 1977-12-13 Coherent Radiation Apparatus for tracking moving workpiece by a laser beam
US4079038A (en) * 1976-03-05 1978-03-14 Alza Corporation Poly(carbonates)
US4066747A (en) * 1976-04-08 1978-01-03 Alza Corporation Polymeric orthoesters housing beneficial drug for controlled release therefrom
US4070347A (en) * 1976-08-16 1978-01-24 Alza Corporation Poly(orthoester) co- and homopolymers and poly(orthocarbonate) co- and homopolymers having carbonyloxy functionality
US4285987A (en) * 1978-10-23 1981-08-25 Alza Corporation Process for manufacturing device with dispersion zone
US4200098A (en) * 1978-10-23 1980-04-29 Alza Corporation Osmotic system with distribution zone for dispensing beneficial agent
US4434153A (en) * 1982-03-22 1984-02-28 Alza Corporation Drug delivery system comprising a reservoir containing a plurality of tiny pills
US4421736A (en) * 1982-05-20 1983-12-20 Merrel Dow Pharmaceuticals Inc. Sustained release diethylpropion compositions
US4721613A (en) * 1982-12-13 1988-01-26 Alza Corporation Delivery system comprising means for shielding a multiplicity of reservoirs in selected environment of use
US4508728A (en) * 1984-05-24 1985-04-02 Kineshiro Nagai Method of treating inflammatory diseases
ES2061442T3 (es) * 1985-10-14 1994-12-16 Nippon Zoki Pharmaceutical Co Peptidos.
DE3703938A1 (de) * 1986-02-12 1987-09-10 Mitsubishi Electric Corp Teilchenbeschleuniger
US4820523A (en) * 1986-04-15 1989-04-11 Warner-Lambert Company Pharmaceutical composition
US4752470A (en) * 1986-11-24 1988-06-21 Mehta Atul M Controlled release indomethacin
US4816263A (en) * 1987-10-02 1989-03-28 Alza Corporation Dosage form for treating cardiovascular diseases comprising isradipine
US4908353A (en) * 1987-10-16 1990-03-13 Nippon Zoki Pharmaceutical Co., Ltd. Novel dipeptide useful as a plant growth regulator
US4853229A (en) * 1987-10-26 1989-08-01 Alza Corporation Method for adminstering tiny pills
US5094848A (en) * 1989-06-30 1992-03-10 Neorx Corporation Cleavable diphosphate and amidated diphosphate linkers
US5084479A (en) * 1990-01-02 1992-01-28 Warner-Lambert Company Novel methods for treating neurodegenerative diseases
US6197819B1 (en) * 1990-11-27 2001-03-06 Northwestern University Gamma amino butyric acid analogs and optical isomers
WO1992009560A1 (en) 1990-11-27 1992-06-11 Northwestern University Gaba and l-glutamic acid analogs for antiseizure treatment
DK0641330T3 (da) 1992-05-20 2001-12-03 Univ Northwestern Gaba- og L-glutaminsyreanaloger til antikrampeanfaldsbehandling
RU2107691C1 (ru) * 1995-03-02 1998-03-27 Дейгин Владислав Исакович Пептид и способ его получения
DE69712877T2 (de) 1996-02-07 2002-11-14 Warner-Lambert Co., Morris Plains Zyklischaminosäure als pharmazeutische mittel
DK0888286T3 (da) 1996-03-14 2002-02-18 Warner Lambert Co Nye substituerede cykliske aminosyrer som farmaceutiske midler
EA001214B1 (ru) 1996-03-14 2000-12-25 Варнер-Ламберт Компани Новые мостиковые циклические аминокислоты как фармацевтически применимые вещества
EP0934061B3 (en) * 1996-07-24 2015-01-21 Warner-Lambert Company LLC Isobutylgaba and its derivatives for the treatment of pain
US6375987B1 (en) * 1996-10-01 2002-04-23 Gattefossé, S.A. Process for the manufacture of pharmaceutical composition with modified release of active principle comprising the matrix
NZ334898A (en) 1996-10-23 2000-09-29 Warner Lambert Co Substituted gamma aminobutyric acids as pharamceutical agents
AU8668598A (en) 1997-08-20 1999-03-08 University Of Oklahoma, The Gaba analogs to prevent and treat gastrointestinal damage
ATE323067T1 (de) 1997-10-27 2006-04-15 Warner Lambert Co Zyklische aminosäuren und deren derivate als arzneimittel
CN1279667A (zh) 1997-12-16 2001-01-10 沃尼尔·朗伯公司 4(3)取代-4(3)-氨基甲基-(硫代)吡喃(噻喃)或-哌啶衍生物(=加巴喷丁类似物)、其制备及其在治疗神经病方面的用途
WO1999031074A2 (en) 1997-12-16 1999-06-24 Warner-Lambert Company ((cyclo)alkyl substituted)-.gamma.-aminobutyric acid derivatives (=gaba analogues), their preparation and their use in the treatment of neurological disorders
NZ503963A (en) 1997-12-16 2002-09-27 Warner Lambert Co 1-substituted-1-aminomethyl-cycloalkane derivatives, or gabapentin analogues, preparation and use in the treatment of neurological disorders
CA2309354A1 (en) 1998-01-23 1999-07-29 Leslie Magnus-Miller Gabapentin and its derivatives for the treatment of muscular and skeletal pain
JP2002516312A (ja) 1998-05-26 2002-06-04 ワーナー−ランバート・カンパニー カルシウムチャンネルのα2δサブユニットに対する親和性を有する立体配座的に制約されたアミノ酸化合物
FR2779651B1 (fr) * 1998-06-16 2001-04-20 Gattefosse Ets Sa Procede pour la fabrication de comprimes a liberation prolongee de principe(s) actif(s) presentant une cinetique de dissolution d'ordre zero
US6171615B1 (en) * 1998-07-06 2001-01-09 Gattefoss{acute over (e)} Sustained release theophylline formulations, excipient systems and methods of production
NZ510145A (en) 1998-09-14 2003-02-28 Warner Lambert Co Branched alkyl pyrrolidine-3-carboxylic acids useful in protective action against cardiazole cramp and cerebral conditions such as epilepsy, hypokinesia and cranial traumas
WO2000023067A1 (en) 1998-10-16 2000-04-27 Warner-Lambert Company Method for the treatment of mania and bipolar disorder
WO2000031020A1 (en) 1998-11-25 2000-06-02 Warner-Lambert Company Improved gamma amino butyric acid analogs
EP1031350A1 (en) 1999-02-23 2000-08-30 Warner-Lambert Company Use of a gabapentin-analog for the manufacture of a medicament for preventing and treating visceral pain
AU7703400A (en) 1999-09-14 2001-04-17 Xenoport, Inc. Substrates and screening methods for transport proteins
GB2362646A (en) 2000-05-26 2001-11-28 Warner Lambert Co Cyclic amino acid derivatives useful as pharmaceutical agents
NZ522480A (en) 2000-06-26 2005-06-24 Warner Lambert Co Gabapentin analogues for sleep disorders
GB2365425A (en) 2000-08-01 2002-02-20 Parke Davis & Co Ltd Alkyl amino acid derivatives useful as pharmaceutical agents
WO2002044324A2 (en) 2000-10-06 2002-06-06 Xenoport, Inc. Bile-acid derived compounds for enhancing oral absorption and systemic bioavailability of drugs
AU2002230398A1 (en) * 2000-10-06 2002-04-29 Xenoport, Inc. Bile-acid conjugates for providing sustained systemic concentrations of drugs
US20020151526A1 (en) 2000-10-06 2002-10-17 Gallop Mark A. Bile-acid prodrugs of L-dopa and their use in the sustained treatment of parkinsonism
WO2002028881A1 (en) 2000-10-06 2002-04-11 Xenoport, Inc. Bile-acid derived compounds for providing sustained systemic concentrations of drugs after oral administration
AU2002239257A1 (en) 2000-11-17 2002-06-03 Xenoport, Inc. Amino acid conjugates providing for sustained systemic concentrations of gaba analogues
EP1412324A4 (en) * 2001-06-11 2004-09-29 Xenoport Inc AMINO ACID CONJUGATES THAT RESULT IN GABA ANALOGA LASTING SYSTEMIC CONCENTRATIONS
AU2002310409C1 (en) * 2001-06-11 2008-04-17 Xenoport, Inc. Orally administered dosage forms of GABA analog prodrugs having reduced toxicity

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007506729A (ja) * 2003-09-25 2007-03-22 ワーナー−ランバート カンパニー リミテッド ライアビリティー カンパニー α2δタンパク質に親和性を有するアミノ酸のプロドラッグ
US8251059B2 (en) 2006-06-27 2012-08-28 Otsuka Pharmaceutical Co., Ltd. Powder inhaler
JP2013518897A (ja) * 2010-02-03 2013-05-23 エムイーエイチ アソシエイツ,インコーポレイテッド 選択的および生体活性的等配電子体としての多重置換フルオロメタン

Also Published As

Publication number Publication date
US20030181390A1 (en) 2003-09-25
WO2002100344A2 (en) 2002-12-19
EP1412324A2 (en) 2004-04-28
US7420002B2 (en) 2008-09-02
AU2002345638A1 (en) 2002-12-23
US7645797B2 (en) 2010-01-12
US20040254344A1 (en) 2004-12-16
EP1412324A4 (en) 2004-09-29
WO2002100344A3 (en) 2004-02-12
US20080226716A1 (en) 2008-09-18

Similar Documents

Publication Publication Date Title
US7645797B2 (en) Amino acid conjugates providing for sustained systemic concentrations of GABA analogues
US7767649B2 (en) Amino acid conjugates providing for sustained systemic concentrations of GABA analogues
US7049305B2 (en) Bile-acid conjugates providing for sustained systemic concentration of drugs
US6992076B2 (en) Bile-acid derived compounds for providing sustained systemic concentrations of drugs after oral administration
EP2109465B1 (en) Polar hydrophilic prodrugs of amphetamine and other stimulants and processes for making and using the same
CA2942724C (en) Tco conjugates and methods for delivery of therapeutic agents
WO2002042414A2 (en) Amino acid conjugates providing for sustained systemic concentrations of gaba analogues
CA2649360A1 (en) Mono and di-substituted oxycodone compounds and compositions
EP2994152B1 (de) Konjugate zum schutz vor nephrotoxischen wirkstoffen
EP2994153A1 (de) Peptide und peptid-wirkstoff-konjugate für renales targeting
EP1991248B1 (en) Antidepressant prodrugs
US20070099841A1 (en) Prodrugs of T3 and T4 with enhanced bioavailability
TW383337B (en) Process of making (2S,5S)-5-fluoromethylornithine
Gao Design, Synthesis and Evaluation of Dipeptides as Probes for Studies of Gastrointestinal Tract Dipeptide Transport System

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20050608

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20050608

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20090612

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20091120